- SUBSTITUTED OXADIAZOLE CHEMICAL COMPOUND AND COMPOSITION CONTAINING SAID CHEMICAL COMPOUND AND USE THEREOF
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Provided are a substituted oxadiazole chemical compound and composition containing said chemical compound and use thereof; said substituted oxadiazole chemical compound is the oxadiazole chemical compound as represented by formula (I), or its crystalline form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate, or solvent compound. The disclosed substituted oxadiazole chemical compound and composition containing said chemical compound are capable of inhibiting indoleamine 2,3-dioxygenase; it also has better pharmacokinetic parameter attributes and is capable of improving the drug concentration of the chemical compound in an animal body, thus improving the therapeutic efficacy and safety of the drug.
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Paragraph 0038; 0039
(2018/11/21)
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- Derivatives and application to the asymmetric synthesis of unnatural α-amino acid derivative
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We describe herein a manganese(IV) oxide-mediated oxidation of N-p-methoxyphenyl (PMP)-protected glycine derivatives for the synthesis of a-imino carboxylic acid derivatives. Using this methodology, utilization of unstable glyoxic acid derivatives was avoided. Furthermore, using this methodology we synthesized novel a-imino carboxylic acid derivatives such as a-imino phenyl ester, perfluoroalkyl etsers, imides, and thioester. The asymmetric Mannich reaction of those novel imine derivatives with 1,3-dicarbonyl compound is also described, and the novel a-imino imide gave improved chemical yield and stereoselectivity compared with those obtained by the use of the conventional a-imino ester-type substrate.
- Inokuma, Tsubasa,Jichu, Takahisa,Nishida, Kodai,Shigenaga, Akira,Otaka, Akira
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p. 573 - 581
(2017/06/07)
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- A convenient method for preparation of α-imino carboxylic acid derivatives and application to the asymmetric synthesis of unnatural α-amino acid derivative
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We describe herein a manganese(IV) oxide-mediated oxidation of N-p-methoxyphenyl (PMP)-protected glycine derivatives for the synthesis of α-imino carboxylic acid derivatives. Using this methodology, utilization of unstable glyoxic acid derivatives was avo
- Inokuma, Tsubasa,Jichu, Takahisa,Nishida, Kodai,Shigenaga, Akira,Otaka, Akira
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p. 573 - 581
(2019/12/26)
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- Preparations, X-ray crystal structure determinations, and base strength measurements of substituted tritylamines
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A range of tritylamines TrNRR′, and 4-methoxy-, 4,4′-dimethoxy-, and 4,4′,4″-trimethoxy-substituted analogues, have been prepared from (substituted) trityl chloride, bromide, or tetrafluoroborate with ammonia or with amines HNRR′ where R and R′ are hydrog
- Canle, Moises L.,Clegg, William,Demirtas, Ibrahim,Elsegood, Mark R.J.,Maskill, Howard
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